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What is Ketoconazole?

Ketoconazole is one of the drugs that plays an important role in the recovery and control of fungal infections and is known as one of the most effective and important elements in medical science. Ketoconazole is an effective antifungal from the azole family that is used to treat fungal infections in humans. This drug works by inhibiting the growth and development of fungi by inhibiting the production mechanisms of sfetosterol, an essential substance for the health of fungal cells. In the following, we will examine the uses, pharmaceutical forms, how to use in children and adults, cautions, etc. Ketoconazole drug.

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Pharmaceutical forms of ketoconazole

Ketoconazole is available in the market as a regular tablet of 200 mg, lotion, cream and shampoo. Also, the drugs of this group are fluconazole, itraconazole, posaconazole, voriconazole, isaconazole, etc.

Uses of Ketoconazole

This medicine is used to treat a specific skin disease (seborrheic dermatitis, a type of dandruff). In this condition, a fungus (Malassezia furfur) is believed to infect the skin or scalp, resulting in dry, scaly skin (scales) or scalp, face, ears, chest, or upper back. Ketoconazole is an azole antifungal drug that works by stopping the growth of fungi. Some of the uses of this drug include fungal infections, Cushing’s syndrome (off the label), recurrent tinea versicolor (off the label) and…

Pharmacological effects and mechanism of action of Ketoconazole drug

Ketoconazole’s mechanism of action inhibits cytochrome P450-dependent ergosterol synthesis, which in turn prevents cell membrane formation. Cushing’s syndrome (off-label) is due to inhibition of P450 enzymes involved in the first step in cortisol synthesis, cleaving the cholesterol side chain and converting 11-deoxycortisol to cortisol. This drug is well distributed in inflamed joint fluid, saliva, bile, urine, breast milk, sebum, cerumen, feces, tendons, skin and soft tissue, testicles. It crosses the weak blood-brain barrier and only small amounts reach the CSF. It is excreted through feces (57%) and urine (13%).

Dosage of Ketoconazole

Before starting to use ketoconazole, read the instructions on the package. If you have any questions, ask your doctor or pharmacist. Use this medicine only on the skin or scalp. If you use the ointment or cream of this medicine, first clean and dry the desired area and then wash your hands before and after using this medicine. Apply this medicine on the affected skin and also on a small amount of normal skin next to this area, as directed by the doctor, once a day. The length of treatment depends on the type of inflammation and response to treatment, which is usually 2 weeks.

Time to take ketoconazole tablets

Take Ketoconazole cream or lotion as directed by your doctor and do not exceed the prescribed amount. If you take too much or too much, your condition will not improve faster, but the side effects may increase. Do not use this medicine in the eyes, nose or mouth, if it comes in contact with it, wash it with plenty of water. If irritation occurs, contact your doctor immediately. Use this medicine regularly to get the most benefit from it. Also, do not wash the treated area for at least 3 hours after using this medicine.

Dosage of ketoconazole in adults

  1. It is recommended for the treatment of systemic fungal infections (eg, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis) in patients who have failed or are intolerant to other therapies. The recommended dose is 200 to 400 mg.
  2. This drug is used to inhibit steroidogenesis in patients with Cushing’s syndrome, the recommended dose is 600-800 mg per day. Also, ketoconazole is rarely and often toxic in the doses needed to reduce cortisol secretion.
  3. In patients with hepatic impairment, no dose modification is provided in the manufacturer’s label. If hepatotoxicity occurs during treatment, discontinue the dose and perform a complete set of liver tests.
  4. Do not use pills as a primary treatment. This drug should be used only when other effective antifungal treatments are not available or the potential benefit outweighs the potential for hepatotoxicity.
  5. Avoid prescribing pills to treat fungal skin and nail infections due to the risk of serious liver damage, adrenal gland problems, and harmful interactions.

Dosage of ketoconazole in children

  1. It is used to treat systemic fungal infections (eg, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis) in patients who have failed or are intolerant to other therapies. The recommended dose in children over 2 years old is 3.3 to 6.6 mg/kg.
  2. In children, this drug should be prescribed with caution and based on weight. Also, this drug is not used as a primary drug and should be prescribed if necessary.


Before using ketoconazole, if you are allergic to it or other azole antifungals such as clotrimazole, econazole, or miconazole, avoid using it. This drug may contain inactive ingredients that may cause allergic reactions or other problems in some patients. If you have a medical history or special sensitivity, consult your doctor regarding possible risks and complications. During pregnancy, this drug should be used only when the drug is clearly needed, because its ingredients can cause risks to the baby and fetus.

  1. Do not use Ketoconazole as primary treatment. It should be used only when other effective antifungal therapies are not available or tolerated and the potential benefit outweighs the potential for hepatotoxicity.
  2. Avoid prescribing pills to treat fungal skin and nail infections due to the risk of serious liver damage, adrenal gland problems, and harmful interactions with other medications that outweigh the benefits of treating these conditions.
  3. Use with caution in patients allergic to other azoles.
  4. Increased long bone fragility has been reported with high doses in animal studies. Choose the dose carefully in patients prone to bone fragility, including the elderly and postmenopausal women.
  5. Decreased absorption has been reported in patients with achlorhydria. Avoid simultaneous use with drugs that reduce stomach acidity.
  6. Hepatotoxicity has been reported in some patients (including death or liver transplantation).
  7. Concomitant use of HMG-CoA reductase inhibitors metabolized by CYP3A4 (eg, simvastatin, lovastatin) increases the risk of myopathy.

Ketoconazole contraindications

  1. Hypersensitivity
  2. Contraindicated with dofetilide, quinidine, pimozide, cisapride, methadone, disopyramide, drondarone and ranolazine and can increase the plasma concentration of these drugs and prolong the QT intervals, which sometimes leads to life-threatening ventricular rhythm disorders (such as Torsade de Pointe). .
  3. Concomitant treatment with cisapride, ergot derivatives or triazolam (fatal cardiac arrhythmias may occur)
  4. Acute or chronic liver disease
  5. CYP3A4 Inhibitors of metabolized HMG-CoA reductase (eg, simvastatin, lovastatin), ketoconazole inhibits CYP3A4 and may increase the risk of statin-associated myopathy.

Warnings and risks of using ketoconazole tablets

  1. Tablets should be used only when other effective antifungal treatments are not available or tolerated and the potential benefits outweigh the potential risks.
  2. Oral hepatotoxicity (including cases of death or need for liver transplantation) has occurred. Also, some patients had no obvious risk factors for liver disease.
  3. In some patients it may cause QT prolongation. Simultaneous use with doftilide, quinidine, pimozide, cisapride, methadone, disopyramide, drondarone and ranolazine is contraindicated. Ketoconazole can increase plasma concentrations of these drugs (by inhibiting CYP3A4) and prolong QT intervals, sometimes leading to life-threatening ventricular arrhythmias such as torsade de pointes.

Ketoconazole side effects

Burning, redness or dryness of the skin in cream or lotion and nausea and vomiting, abdominal pain, headache and dizziness, fever and drowsiness are side effects of Ketoconazole tablets. If any of the side effects of this drug worsen, stop using the drug and inform the doctor. Most people who use this drug do not experience serious side effects. Some of its serious side effects include blisters or open sores on the treated skin, eye swelling, liver toxicity, etc. If any of these occur, see a doctor.

  1. nausea and vomiting
  2. itching
  3. stomach ache
  4. Headache and dizziness
  5. Hyperlipidemia
  6. Drowsiness
  7. Ague
  8. depression
  9. Gynecomastia
  10. diarrhea
  11. impotence

Ketoconazole shampoo for dandruff

Ketoconazole drug interactions

Drug interactions may change how your medications work or increase your risk of serious side effects. These interactions occur in chemical or herbal medicines. Ketoconazole drug interacts with hepatotoxic drugs, anticholinergic antacids, antispasmodics, statins, H2 receptor antagonists, omeprazole, sucralfate, astemizole, cisapride, cyclosporine, isoniazid, rifampin, phenytoin and warfarin.

Taking Ketoconazole tablets during pregnancy and breastfeeding

Ketoconazole drug is in category C of risks during pregnancy, that is, it can be used in special conditions and under the special supervision of a doctor. Animal studies on this drug have shown few risks, and specific human studies are not available. The benefits of the drug against possible risks and side effects determine whether or not to use this drug during pregnancy.

Ketoconazole storage conditions

Ketoconazole medicine should be stored at room temperature and away from heat or high temperature, because this medicine is flammable. Keep all medicines out of the reach of children and animals. If you intend to dispose of the medicine, dispose of it according to hygiene principles.

A final word about ketoconazole

In this article from the online positive pharmacy magazine, we carefully reviewed the drug ketoconazole, one of the effective azole drugs in the treatment of fungal infections in humans. By inhibiting the mechanism of sfetosterol production in fungi, this drug has been proven as an effective substance for skin health and as an effective means of fighting fungal infections. The benefits of ketoconazole, including its therapeutic efficacy and wide range of applications in the treatment of various fungal infections, are of great importance in medical science.

Site source: Medscape

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